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    Title: Synthesis of a Lipid/Peptide/Drug Conjugate : N4-(Acylpeptidyl)-Ara-C
    Authors: 李世元;Lee, Adam Shih-yuan;Menger, F. M.;Guo, Y.
    Contributors: 淡江大學化學學系
    Date: 1994-03-01
    Issue Date: 2009-12-01
    Publisher: American Chemical Society (ACS)
    Abstract: A lipidlpeptideldrug conjugate, N4-(acylpeptidyl)-ara-C, is synthesized under mild conditions to give an ara-C prodrug protected against cytidine deaminase-catalyzed deactivation. The compounds can be bound, via their hydrocarbon tails, to phospholipid membranes and examined for chymotrypsininduced drug release. A tripeptide is too short to permit efficient enzymelmembrane contact and subsequent freeing of the drug. Faster rates can, presumably, be achieved by "fine tuning" the length and polarity of the peptide spacer attached to the drug.
    Relation: Bioconjugate Chemistry 5(2), pp.162-166
    DOI: 10.1021/bc00026a601
    Appears in Collections:[化學學系暨研究所] 期刊論文

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